二氢链霉素的1-和3-脱脒基衍生物以及一些1-N-酰基衍生物。

1- and 3-deamidino derivatives of dihydrostreptomycin and some 1-N-acyl derivatives.

作者信息

Usui T, Tsuchiya T, Umezawa S

出版信息

J Antibiot (Tokyo). 1978 Oct;31(10):991-6. doi: 10.7164/antibiotics.31.991.

DOI:10.7164/antibiotics.31.991

Abstract

1-Deamidino-, 3-deamidino- and 1,3-di(deamidino)dihydrostreptomycin (1, 2, 3) were prepared by treatment of dihydrostreptomycin (DHSM) with ammonia at 100 degrees C. The 3-guanidino group of DHSM is suggested to be more important than the 1-guanidino group for the antibacterial activity of DHSM. 1-N-[(S)-4-Amino-2-hydroxybutyryl) and 1-N-[(S)-4-guanidino-2-hydroxybutyryl] derivatives (4, 6) of 1-deamidinodihydrostreptomycin were futher prepared.

摘要

通过在100℃下用氨处理二氢链霉素（DHSM）制备了1-脱脒基-、3-脱脒基-和1,3-二（脱脒基）二氢链霉素（1、2、3）。对于DHSM的抗菌活性，有人认为DHSM的3-胍基比1-胍基更重要。进一步制备了1-脱脒基二氢链霉素的1-N-[(S)-4-氨基-2-羟基丁酰基]和1-N-[(S)-4-胍基-2-羟基丁酰基]衍生物（4、6）。